Pyridoxine hydroxamic acids as novel HIV-integrase inhibitors

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1233-6. doi: 10.1016/j.bmcl.2016.01.028. Epub 2016 Jan 20.

Abstract

A series of pyridoxine hydroxamic acid analog bearing a 5-aryl-spacers were synthesized. Evaluation of these novel HIV integrase complex inhibitors revealed compounds with high potency against wild-type HIV virus.

Keywords: Active site binding; HIV integrase inhibitor; Hydroxamic acid; Pyridoxine.

MeSH terms

  • Animals
  • Catalytic Domain
  • Female
  • HIV Integrase / chemistry*
  • HIV Integrase / metabolism
  • HIV Integrase Inhibitors / chemical synthesis
  • HIV Integrase Inhibitors / chemistry*
  • HIV Integrase Inhibitors / pharmacokinetics
  • HIV-1 / physiology*
  • Half-Life
  • Humans
  • Hydroxamic Acids / chemical synthesis
  • Hydroxamic Acids / chemistry*
  • Hydroxamic Acids / pharmacokinetics
  • Inhibitory Concentration 50
  • Pyridoxine / chemistry
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship
  • Virus Replication / drug effects

Substances

  • HIV Integrase Inhibitors
  • Hydroxamic Acids
  • HIV Integrase
  • Pyridoxine